1 Curriculum Vitae Dr. Raymond J. Bergeron Distinguished ...

Education:
Curriculum Vitae
Dr. Raymond J. Bergeron
Distinguished Professor Emeritus
University of Florida
Clark University A.B. 1967 Chemistry
Brandeis University Ph.D. 1972 Chemistry
Harvard University Fellow 1972–74 K. Bloch (Nobel Laureate)
Research/Professional Experience:
2001 to 2012: Duckworth Eminent Scholar
1996 to 2000: Duckworth Professor of Drug Development
1/92 to 2012: Graduate Research Professor, Medicinal Chemistry
University of Florida
3/83 to 1/92: Prof. of Medicinal Chemistry, Chemistry and Medicine
University of Florida
1/79 to 3/83: Assoc. Prof., Medicinal Chemistry, College of Pharmacy with
Appointments in: Dept. of Chemistry, College of Arts and
Sciences; Dept. of Medicine, College of Medicine, University of Florida
6/78 to 9/78: Visiting Scientist, National Institutes of Health
7/74 to 12/78: Assist. Prof., Dept. of Chemistry, College of Arts and Sciences,
University of Maryland
Distinctions:
• NASA Fellowship (Brandeis University)
• NIH Postdoctoral Fellowship (Harvard University)
• Sloan Foundation Fellowship (University of Maryland)
• National Institutes of Health Medicinal Chemistry Study Section Member
• Editorial Board - Journal of Inclusion Phenomena
• Advisor - Iron Overload Foundation
• Florida Scientist of the Year (1989)
• Graduate Research Professor (1992–2012)
• Duckworth Professor of Drug Development (1996–2000)
• Duckworth Eminent Scholar (2000–2012)
• University of Florida Research Foundation Professorship (2001–2004)
• NIH MERIT Award - (2005–2015)
1

Consultant Positions:
• Ciba-Geigy Pharmaceuticals, Basel, Switzerland
• Emisphere Technologies Associates Inc., Hawthorne, NY
• SunPharm Corporation, Ponte Vedra, FL
• Parke-Davis/Warner-Lambert, Ann Arbor, MI
• GelTex Pharmaceuticals, Waltham, MA
• Genzyme, Cambridge, MA
• Sun BioPharma, LLC, Ponte Vedra Beach, FL
Journal Articles and Chapters:
1. “Protection and Monoalkylation of Amines.” J. B. Hendrickson and R. J. Bergeron,
Tetrahedron Lett., 11(5), 345–348 (1970).
2. “Triflamides (CF3SO2N). A Survey.” J. B. Hendrickson, R. J. Bergeron, A. Giga, and D.
Sternbach, J. Am. Chem. Soc., 95, 3412–3413 (1973).
3. “A New Thermal Pericyclic Carbon Transfer Capable of Creating Quaternary Sites.”
J. B. Hendrickson and R. J. Bergeron, Tetrahedron Lett., 14(37), 3609–3610 (1973).
4. “Triflamides for Protection and Monoalkylation of Amines and a New Gabriel Synthesis.” J.
B. Hendrickson and R. J. Bergeron, Tetrehedron Lett., 14(39), 3839–3842 (1973).
5. “Triflamides: New Acylating and Triflating Reagents.” J. B. Hendrickson and R. J.
Bergeron, Tetrahedron Lett., 14(46), 4607–4610 (1973).
6. “Effects of Cyclodextrins on Fatty Acid Synthesis.” Y. Machida, R. J. Bergeron, P. Flick,
and K. Bloch, J. Biol. Chem., 248, 6246–6247 (1973).
7. “New ‘Gabriel’ Syntheses of Amines.” J. B. Hendrickson, R. J. Bergeron, and D. D.
Sternbach, Tetrahedron, 31, 2517–2521 (1975).
8. “Complex Formation Between Mycobacterial Polysaccharides or Cyclodextrins and
Palmitoyl Coenzyme A.” R. J. Bergeron, Y. Machida, and K. Bloch, J. Biol. Chem., 250,
1223–1230 (1975).
9. “Selective Alkylation of Cycloheptaamylose.” R. J. Bergeron, M. Meeley, and Y.
Machida, Bioorg. Chem., 5, 121–126 (1976).
10. “The Role of Strain Energy in Cycloamylose Substrate Complexation.” R. J. Bergeron and
M. Meeley, Bioorg. Chem., 5, 197–202 (1976).
11. “The Molecular Disposition of Sodium p-Nitrophenolate in the Cavities of
Cycloheptaamylose and Cyclohexaamylose in Solution.” R. J. Bergeron and R.
Rowan, III, Bioorg. Chem., 5, 425–436 (1976).
2

12. “The Molecular Disposition of p-Nitrophenol and Sodium p-Nitrophenolate in the
Cyclohexaamylose Cavity: A 13 C Probe.” R. J. Bergeron and M. A. Channing, Bioorg.
Chem., 5, 437–439 (1976).
13. “Cycloamyloses.” R. J. Bergeron, J. Chem. Ed., 54, 204–207 (1977).
14. “Disposition Requirements for Binding in Aqueous Solution of Polar Substrates in the
Cyclohexaamylose Cavity.” R. J. Bergeron, M. A. Channing, G. J. Gibeily, and D. M. Pillor,
J. Am. Chem. Soc., 99, 5146–5151 (1977).
15. “Circular Dichroism Studies on the Structure of p-Nitrophenolate Cycloamylose
Complexes.” R. J. Bergeron and P. McPhie, Bioorg. Chem., 6, 465–471 (1977).
16. “Uses of the Trifyl [trifluoromethanesulfonyl] Group in Organic Synthesis. A
Review.” J. B. Hendrickson, K. W. Bair, R. J. Bergeron, A. Giga, P. L. Skipper, D. D.
Sternbach, and J. A. Wareing, Org. Prep. Proc. Int., 9, 173–207 (1977).
17. “Thermodynamics of Cycloamylose-Substrate Complexation.” R. J. Bergeron, D. M. Pillor,
G. Gibeily, and W. P. Roberts, Bioorg. Chem., 7, 263–271 (1978).
18. “Dependence of Cycloamylose-Substrate Binding on Charge.” R. J. Bergeron, M. A.
Channing, and K. A. McGovern, J. Amer. Chem. Soc., 100, 2878–2883 (1978).
19. “Boundary Conditions for the Hildebrand-Benesi Equation.” R. J. Bergeron and W. P.
Roberts, Anal. Biochem., 90, 844–848 (1978).
20. “Mild Oxidation of Alkyl Halides.” R. J. Bergeron and P. G. Hoffman, J. Org. Chem., 44,
1835–1839 (1979).
21. “Carboxylate Anion Binding in the Cyclohexaamylose Cavity: A Steric and Electronic
Evaluation.” R. J. Bergeron, M. A. Channing, K. A. McGovern, and W. P. Roberts, Bioorg.
Chem., 8, 263–281(1979).
22. “Importance of Cycloamylose Substrate Geometry and Dynamic Coupling in the
Deacylation of 3- and 4-Nitrophenyl Acetates.” R. J. Bergeron and M. A. Channing, J.
Am. Chem. Soc., 101, 2511–2516 (1979).
23. “Application of N-Phenyltrifluoromethanesulfonamides to the Synthesis of Pyrazines.” R. J.
Bergeron and P. G. Hoffman, J. Org. Chem., 45, 161–163 (1980).
24. “Application of N-Phenyltriflamide to the Synthesis of Deoxyaspergillic Acid." R. J.
Bergeron and P. G. Hoffman, J. Org. Chem., 45, 163–165 (1980).
25. “Synthesis of N 4 -Acylated N 1 ,N 8 -Bis(acyl)spermidines: An Approach to the Synthesis of
Siderophores.” R. J. Bergeron, K. A. McGovern, M. A. Channing, and P. S. Burton, J. Org.
Chem., 45,1589–1592 (1980).
3

26. “Synthesis, Absorption and Toxicity of N 1 ,N 8 -Bis(2,3-dihydroxybenzoyl)spermidine, a
Potent Iron Chelator.” R. J. Bergeron, P. S. Burton, K. A. McGovern, E. J. St. Onge, and R.
R. Streiff, J. Med. Chem., 23, 1130–1133 (1980).
27. “Biomimetic Synthesis of a Paracoccus denitrificans Siderophore Analogue.” R. J.
Bergeron, P. S. Burton, S. J. Kline, and K. A. McGovern, J. Org. Chem., 46, 3712–3718
(1981).
28. “Reagents for the Selective Acylation of Spermidine, Homospermidine and Bis[3-aminopropyl]-amine.”
R. J. Bergeron, P. S. Burton, K. A. McGovern, and S. J. Kline, Synthesis,
732–733 (1981).
29. “Flexible Synthesis of Polyamine Catecholamides.” R. J. Bergeron, S. J. Kline, N. J.
Stolowich, K. A. McGovern, and P. S. Burton, J. Org. Chem., 46, 4524–4529 (1981).
30. “Role of Cyclohexaamylose C-3 Hydroxyls in Catalytic Hydrolysis.” R. J. Bergeron and P.
S. Burton, J. Am. Chem. Soc., 104, 3664–3670 (1982).
31. “Fluorescent Lipoprotein Probe.” R. J. Bergeron and J. Scott, Anal. Biochem., 119, 128–134
(1982).
32. “Cholestatriene and Ergostatetraene as in vivo and in vitro Membrane and Lipoprotein
Probes.” R. J. Bergeron and J. Scott, J. Lipid Res., 23, 391–404 (1982).
33. “Short Synthesis of Parabactin.” R. J. Bergeron and S. J. Kline, J. Am. Chem. Soc., 104,
4489–4492 (1982).
34. “Biological Properties of N 4- Spermidine Derivatives and their Potential in Anticancer
Chemotherapy.” C. W. Porter, R. J. Bergeron, and N. J. Stolowich, Cancer Res., 42, 4072–
4078 (1982).
35. “Reagents for the Selective Secondary N-Acylation of Linear Triamines.” R. J.
Bergeron, N. J. Stolowich, and C. W. Porter, Synthesis, 689–692 (1982).
36. “Spermidine Requirement for Cell Proliferation in Eukaryotic Cells: Structural
Specificity and Quantitation.” C. W. Porter and R. J. Bergeron, Science, 219, 1083–1085
(1983).
37. “Synthesis and Solution Dynamics of Agrobactin A.” R. J. Bergeron, N. J. Stolowich, and S.
J. Kline, J. Org. Chem., 48, 3432–3439 (1983).
38. “Bacteriostatic and Fungostatic Action of Catecholamide Iron Chelators.” R. J.
Bergeron, G. S. Elliott, S. J. Kline, R. Ramphal, and L. St. James, III, Antimicrob. Agents
Chemother., 24, 725-730 (1983).
4

39. “Catecholamide 'H-shaped' Ligands as Actinide Chelators.” R. J. Bergeron, S. J. Kline, J.
Navratil, and C. M. Smith, Radiochim. Acta, 35, 47–51 (1984).
40. “300 MHz 1 H NMR Study of Parabactin and its Gallium(III) Chelate.” R. J. Bergeron and
S. J. Kline, J. Am. Chem. Soc., 106, 3089–3098 (1984).
41. “Amines and Polyamines from Nitriles.” R. J. Bergeron and J. R. Garlich, Synthesis, 782–
784 (1984).
42. “Reagents for the Stepwise Functionalization of Spermidine, Homospermidine and Bis(3aminopropyl)amine.”
R. J. Bergeron, J. R. Garlich, and N. J. Stolowich, J. Org. Chem., 49,
2997–3001 (1984).
43. “Treatment With a-Difluoromethylornithine Plus a Spermidine Analogue Leads to Spermine
Depletion and Growth Inhibition in Cultured L1210 Leukemia Cells.” R. Casero, R. J.
Bergeron, and C. W. Porter, J. Cell. Physiol., 121, 476–482 (1984).
44. “Cycloamylose–Substrate Binding.” R. J. Bergeron, Inclusion Compounds III, Chapter 12,
J. L. Atwood, J. E. D. Davies and D. D. MacNicol, eds. Academic: London, UK (1984).
45. “Aliphatic Chain Length Specificity of the Polyamine Transport System in Ascites L1210
Leukemia Cells.” C. W. Porter, J. Miller, and R. J. Bergeron, Cancer Res., 44, 126–128
(1984).
46. “Antineoplastic and Antiherpetic Activity of Spermidine Catecholamide Iron Chelators.” R.
J. Bergeron, P. F. Cavanaugh, Jr., S. J. Kline, R. G. Hughes, Jr., G. T. Elliott, and C. W.
Porter, Biochem. Biophys. Res. Comm., 121, 848–854 (1984).
47. “Synthesis and Solution Structures of Microbial Siderophores.” R. J. Bergeron, Chem. Rev.,
84, 587–602 (1984).
48. “Biological Properties of N 4 - and N 1 ,N 8 -Spermidine Derivatives in Cultured L1210
Leukemia Cells.” C. W. Porter, P. F. Cavanaugh, N. J. Stolowich, B. Ganis, E. Kelly,
and R. J. Bergeron, Cancer Res., 45, 2050–2057 (1985).
49. “An Efficient Total Synthesis of Agrobactin and its Gallium(III) Chelate.” R. J.
Bergeron, J. S. McManis, J. B. Dionis, and J. R. Garlich, J. Org. Chem., 50, 2780–2782
(1985).
50. “Total Synthesis of Vibriobactin.” R. J. Bergeron, J. R. Garlich, and J. S. McManis,
Tetrahedron, 41, 507–510 (1985).
51. “Mechanism and Stereospecificity of the Parabactin-Mediated Iron-Transport System
in Paracoccus denitrificans.” R. J. Bergeron, J. B. Dionis, G. T. Elliott, and S. J. Kline, J.
Biol. Chem., 260, 13, 7936–7944 (1985).
5

52. “Influence of Iron on in vivo Proliferation and Lethality of L1210 Cells.” R. J. Bergeron, R.
R. Streiff, and G. T. Elliott, J. Nutr., 115, 369–374 (1985).
53. “Characterization of L1210 Cell Growth Inhibition by the Bacterial Iron Chelators
Parabactin and Compound II.” P. F. Cavanaugh, Jr., C. W. Porter, D. Tukalo, O. S.
Frankfurt, Z. P. Pavelic, and R. J. Bergeron, Cancer Res., 45, 4754–4759 (1985).
54. “Methods for the Selective Modification of Spermidine and its Homologues.” R. J.
Bergeron, Accts. Chem. Res., 19, 105–113 (1986).
55. “Iron: A Controlling Nutrient in Proliferative Processes.” R. J. Bergeron, Trends in
Biochem. Sci., 11, 133–136 (1986).
56. “Effects of the Vibrio cholerae Siderophore Vibriobactin on the Growth Characteristics of
L1210 Cells.” R. J. Bergeron, R. Braylan, S. Goldey, and M. J. Ingeno, Biochem.
Biophys. Res. Comm., 136, 273–280 (1986).
57. “Hexahydropyrimidines as Masked Spermidine Vectors in Drug Delivery.” R. J.
Bergeron and H. W. Seligsohn, Bioorg. Chem., 14, 345–355 (1986).
58. “Comparison and Characterization of Growth Inhibition in L1210 Cells by a-
Difluoromethylornithine (DFMO), an Inhibitor of Ornithine Decarboxylase, and
N 1 ,N 8 -Bis(ethyl)Spermidine, an Apparent Regulator of the Enzyme.” C. W. Porter, B.
Ganis, T. Vinson, L. J. Marton, D. L. Kramer, and R. J. Bergeron, Cancer Res., 46, 6279–
6285 (1986).
59. “Catecholamide Chelators for Actinide Environmental and Human Decontamination.”
R. J. Bergeron and J. D. Navratil, Chemical Separations, Volume II, Applications. C. J. King
and J. T. Navratil (Eds.), Litarvan Literature: Denver, CO (1986).
60. “Synthesis of a Parabactin Photoaffinity Label.” R. J. Bergeron, J. B. Dionis, and M. J.
Ingeno, J. Org. Chem., 52, 144–149 (1987).
61. “Synthesis and Properties of Polyamine Catecholamide Chelators.” R. J. Bergeron, Iron
Transport in Microbes, Plants and Animals, Chapter 16, G. Winklemann, D. Vander Helm,
and J. B. Neilands (Eds.), VCH Verlagsgsellschaft/VCH Publishers, 285–315 (1987).
62. “Structural Determinants of Spermidine-DNA Interactions.” P. M. Vertino, R. J.
Bergeron, P. F. Cavanaugh, Jr., and C. W. Porter, Biopolymers, 26, 691–703 (1987).
63. “Relative Abilities of Bis(ethyl) Derivatives of Putrescine, Spermidine, and Spermine to
Regulate Polyamine Biosynthesis and Inhibit L1210 Leukemia Cell Growth.” C. W. Porter,
J. McManis, R. A. Casero, and R. J. Bergeron, Cancer Res., 47, 2821–2825 (1987).
64. “Total Synthesis of (±)-15-Deoxyspergualin.” R. J. Bergeron and J. S. McManis, J. Org.
Chem., 52, 1700–1703 (1987).
6

65. “Microbial Iron Chelator-Induced Cell Cycle Synchronization in L1210 Cells: Potential in
Combination Chemotherapy.” R. J. Bergeron and M. J. Ingeno, Cancer Res., 47, 6010–6016
(1987).
66. “Regulation of Ornithine Decarboxylase Activity by Spermidine and the Spermidine
Analogue N 1 N 8 -Bis(ethyl)Spermidine.” C. W. Porter, F. G. Berger, A. E. Pegg, B. Ganis,
and R. J. Bergeron, Biochem. J., 242, 433–440 (1987).
67. “Synthetic Polyamine Analogues as Antineoplastics.” R. J. Bergeron, A. H. Neims, J. S.
McManis, T. R. Hawthorne, J. R. T. Vinson, R. Bortell, and M. J. Ingeno, J. Med. Chem.,
31, 1183–1190 (1988).
68. “Demonstration of Ferric L-Parabactin Binding Activity in the Outer Membrane of
Paracoccus denitrificans.” R. J. Bergeron, W. R. Weimar, and J. B. Dionis, J.
Bacteriol., 170, 3711–3717 (1988).
69. “Control of Ornithine Decarboxylase Activity in a-Difluoromethylornithine-Resistant
L1210 Cells by Polyamines and Synthetic Analogues.” A. E. Pegg, R. Madhubala, T.
Kameji, and R. J. Bergeron, J. Biol. Chem., 263, 11008–11014 (1988).
70. “Reagents for the Stepwise Functionalization of Spermine.” R. J. Bergeron and J. S.
McManis, J. Org. Chem., 53, 3108–3111 (1988).
71. “Selective Regulation of S-Adenosylmethionine Decarboxylase Activity by the Spermine
Analogue 6-Spermyne.” C. W. Porter, J. S. McManis, D. Lee, and R. J. Bergeron, Biochem.
J., 254, 337–342 (1988).
72. “Enzyme Regulation as an Approach to Interference with Polyamine Biosynthesis—An
Alternative to Enzyme Inhibition.” C. W. Porter and R. J. Bergeron, Adv. Enz. Regul., 27,
57–79 (1988).
73. “Regulation of Polyamine Biosynthetic Activity by Spermidine and Spermine Analogues—
A Novel Antiproliferative Strategy.” C. W. Porter and R. J. Bergeron, Adv. Exp. Med.
Biol., 250, (Progress in Polyamine Research), V. Zappia and A. E. Pegg, Eds., Plenum
Publishing Corp. 677–690 (1988).
74. “Modulation of Polyamine Biosynthesis and Transport by Oncogene Transfection.” B. K.
Chang, P. R. Libby, R. J. Bergeron, and C. W. Porter, Biochem. Biophys. Res. Comm.,
157, 264–270 (1988).
75. “An Efficient Total Synthesis of Desferrioxamine B.” R. J. Bergeron and J. J. Pegram, J.
Org. Chem., 53, 3131–3134 (1988).
76. “Combination Iron Depletion Therapy.” R. Taetle, J. M. Honeysett, and R. J. Bergeron, J.
Nat. Cancer Inst., 81, 1229–1235 (1989).
7

77. “Differential Response to Treatment with the Bis(ethyl)Polyamine Analogues
Between Human Small Cell Lung Carcinoma and Undifferentiated Large Cell Lung
Carcinoma in Culture.” R. A. Casero, Jr., S. J. Ervin, P. Celano, S. B. Baylin, and R. J.
Bergeron, Cancer Res., 49, 639–643 (1989).
78. “Role of the Methylene Backbone in the Antiproliferative Activity of Polyamine
Analogues on L1210 Cells.” R. J. Bergeron, T. R. Hawthorne, J. R. T. Vinson, D. E. Beck,
Jr., and M. J. Ingeno, Cancer Res., 49, 2959–2964 (1989).
79. “Effect of N 1 , N 12 -Bis(ethyl)Spermine and Related Compounds on Growth and
Polyamine Acetylation, Content and Excretion in Human Colon Tumor Cells.” A. E. Pegg,
R. Wechter, R. Pakala, and R. J. Bergeron, J. Biol. Chem., 264, 11744–11749 (1989).
80. “Differential Induction of Spermidine/Spermine N 1 -Acetyltransferase in Human Lung
Cancer Cells by the Bis(ethyl)Polyamine Analogues.” R. A. Casero, Jr., P. Celano, S. J.
Ervin, C. W. Porter, R. J. Bergeron, and P. Libby, Cancer Res., 49, 3829–3833 (1989).
81. “The Total Synthesis of Bisucaberin.” R. J. Bergeron and J. S. McManis, Tetrahedron, 45,
4939–4944 (1989).
82. “Major Increases in Spermidine/Spermine-N 1 -Acetyltransferase Activity by Spermine
Analogues and their Relationship to Polyamine Depletion and Growth Inhibition in L1210
Cells.” P. R. Libby, M. Henderson, R. J. Bergeron, and C. W. Porter, Cancer Res., 49,
6226–6231 (1989).
83. “Correlation Between the Effects of Polyamine Analogues on DNA Conformation and Cell
Growth.” H. S. Basu, B. G. Feuerstein, D. F. Deen, W. P. Lubich, R. J. Bergeron, K.
Samejima, and L. J. Marton, Cancer Res., 49, 5591–5597 (1989).
84. “Structure-Function Correlations of Polyamine Analog-Induced Increases in
Spermidine/Spermine Acetyltransferase Activity.” P. R. Libby, R. J. Bergeron, and C.
W. Porter, Biochem. Pharmacol., 38, 1435–1442 (1989).
85. “Effect of N 1 , N 14 -Bis-(ethyl)-Homospermine on the Growth of U-87 MG and SF-126
Human Brain Tumor Cells.” H. S. Basu, M. Pellarin, B. G. Feuerstein, D. F. Deen, R. J.
Bergeron, and L. J. Marton, Cancer Res., 50, 3137–3140 (1990).
86. “Kinetics of Iron Acquisition from Ferric Siderophores by Paracoccus denitrificans.” R. J.
Bergeron and W. R. Weimar, J. Bacteriol., 172, 2650–2657 (1990).
87. “A Comparative Evaluation of Iron Clearance Models.” R. J. Bergeron, R. R. Streiff,
J. Wiegand, J. R. T. Vinson, G. Luchetta, K. M. Evans, H. H. Peter, and H.-B. Jenny, Ann.
N. Y. Acad. Sci., 612, 378–393 (1990).
8

88. “Combined Regulation of Ornithine and S-Adenosylmethionine Decarboxylases by
Spermine and the Spermine Analogue N 1 ,N 12 -Bis(ethyl)spermine.” C. W. Porter, A. E.
Pegg, B. Ganis, R. Madhabala, and R. J. Bergeron, Biochem. J., 268, 207–212 (1990).
89. “Induction of Spermidine/Spermine N 1 -Acetyltransferase Activity in Chinese-
Hamster Ovary cells by N 1 ,N 11 -Bis(ethyl)norspermine and Related Compounds.” A. E.
Pegg, R. Pakala, and R. J. Bergeron, Biochem. J., 267(3), 331–338 (1990).
90. “The Total Synthesis of Desferrioxamines E and G.” R. J. Bergeron and J. S. McManis,
Tetrahedron, 46, 5881–5888 (1990).
91. “Increase in Spermine Content Coordinated With Siderophore Production in Paracoccus
denitrificans.” R. J. Bergeron and W. R. Weimar, J. Bacteriol., 173, 2238–2243 (1991).
92. “Selective Cellular Depletion of Mitochondrial DNA by the Polyamine Analog, N 1 ,N 12 -
Bis(ethyl)spermine, and its Relationship to Polyamine Structure and Function.” P. M.
Vertino, T. A. Beerman, E. J. Kelly, R. J. Bergeron, and C. W. Porter, Mol. Pharm., 39,
487–494 (1991).
93. “Characterization of Human Spermidine/Spermine N 1 -Acetyltransferase Purified from
Cultured Melanoma Cells.” P. R. Libby, B. Ganis, R. J. Bergeron, and C. W. Porter, Arch.
Biochem. Biophys., 284, 238-244 (1991).
94. “Synthesis of Catecholamide and Hydroxamate Siderophores.” R. J. Bergeron and J. S.
McManis, CRC Handbook on Microbial Iron Chelates 1991, pp. 271–307 (1991).
95. “Evaluation of Desferrithiocin and its Synthetic Analogues as Orally Effective Iron
Chelators.” R. J. Bergeron, J. Wiegand, J. B. Dionis, M. Egli-Karmakka, J. Frei, A.
Huxley-Tencer, and H. H. Peter, J. Med. Chem., 34, 2072–2078 (1991).
96. “The Total Synthesis of Alcaligin.” R. J. Bergeron, J. S. McManis, P.T. Perumal, and
S. E. Algee, J. Org. Chem, 56, 5560–5563 (1991).
97. “The Synthesis and Biological Evaluation of Hydroxamate-Based Iron Chelators.” R.
J. Bergeron, J. Wiegand, J. S. McManis, and P. T. Perumal, J. Med Chem., 34, 3182–3187
(1991).
98. “Cellular Responses to Polyamine Analogues and Inhibitors in Human Pancreatic
Adenocarcinoma Cell Lines.” B. K. Chang, C. W. Porter, and R. J. Bergeron, J.
Cellular Pharmacol. 2, 133–137 (1991).
99. “Correlations Between Polyamine Analog-Induced Increases in Spermidine/Spermine N 1 -
Acetyltransferase Activity, Polyamine Pool Depletion, and Growth Inhibition in Human
Melanoma Cell Lines.” C. W. Porter, B. Ganis, P. R. Libby, and R. J. Bergeron, Cancer
Res., 51, 3715–3720 (1991).
9

100. “A Comparison of the Iron-Clearing Properties of 1,2-Dimethyl-3-hydroxypyrid-4-one, 1,2-
Diethyl-3-hydroxypyrid-4-one, and Deferoxamine.” R. J. Bergeron, R. R. Streiff, J.
Wiegand, G. Luchetta, E. A. Creary, and H. H. Peter, Blood, 79, 1882–1890 (1992).
101. “Regulation of Polyamine Biosynthetic Activity and Homeostasis as a Novel
Antiproliferative Strategy.” C. W. Porter, D. L. Kramer, R. J. Bernacki, and R. J. Bergeron,
Dev. Oncol., 68, 325–344 (1992).
102. “Differential Effects of the Spermine Analog, N 1 N 12 Bis(ethyl) Spermine, on Polyamine
Metabolism and Cell Growth in Human Melanoma Cell Lines and Melanocytes.” N. W.
Shappell, J. T. Miller, R. J. Bergeron and C. W. Porter, Anticancer Res., 12, 1083–1090
(1992).
103. “Antitumor Effects of N-Alkylated Polyamine Analogs in Human Pancreatic
Adenocarcinoma Models.” B. K. Chang, R. J. Bergeron, C. W. Porter, and Y. Liang, Cancer
Chemother. Pharmacol., 30, 179–182 (1992).
104. “Regulatory and Antiproliferative Effects of N-Alkylated Polyamine Analogs in Human
and Hamster Pancreatic Adenocarcinoma Cell Lines.” B. K. Chang, R. J. Bergeron, C.
W. Porter, J. R. T. Vinson, Y. Liang, and P. R. Libby, Cancer Chemother. Pharmacol., 30,
183–188 (1992).
105. “Antitumor Activity of N,N'-Bis(ethyl)spermine Homologues Against Human MALME-3
Melanoma Xenografts.” R. J. Bernacki, R. J. Bergeron, and C. W. Porter, Cancer Res.,
52, 2424-2430 (1992).
106. “Polyamine Analogues in Pancreatic Adenocarcinoma: A Strategy for Effective
Antitumor Therapy in Chemoresistant Gastrointestinal Malignancies.” B. K. Chang, R. J.
Bergeron, C. W. Porter, and J. R. T. Vinson, Falk Symposium on Polyamines in the
Gastrointestinal Tract, 62, 173–186, Kluwer Press, Lancaster, U.K. (1992).
107. “Polyamine Inhibitors and Analogues as Potential Anticancer Agents.” C. W. Porter, U.
Regenass, and R. J. Bergeron, Falk Symposium on Polyamines in the Gastrointestinal Tract,
62, 301–322, Kluwer Press, Lancaster, U.K. (1992).
108. “The Total Synthesis of Nannochelin: A Novel Cinnamoyl Hydroxamate-Containing
Siderophore.” R. J. Bergeron and O. Phanstiel, IV, J. Org. Chem., 57, 7140–7143 (1992).
109. “Structural Alterations in Desferrioxamine Compatible with Iron Clearance in
Animals.” R. J. Bergeron, Z. R. Liu, J. S. McManis, and J. Wiegand, J. Med. Chem.,
35, 4739–4744 (1992).
110. “Steady-State Messenger RNA and Activity Correlates With Sensitivity to N 1 ,N 12 -
Bis(ethyl)spermine in Human Cell Lines Representing the Major Forms of Lung
Cancer.” R. A. Casero, Jr., A. R. Mank, L. Xiao, J. Smith, R. J. Bergeron, and P. Celano,
Cancer Res., 52, 5359–5363 (1992).
10

111. “Regulation of Polyamine Transport by Polyamines and Polyamine Analogs.” D. L.
Kramer, J. T. Miller, R. J. Bergeron, R. Khomutov, A. Khomutov, and C. W. Porter, J. Cell.
Physiol., 155, 399–407 (1993).
112. “Effects of Diethylspermine Analogues in Human Bladder Cancer Cell Lines in
Culture.” B. K. Chang, Y. Liang, D. W. Miller, R. J. Bergeron, C. W. Porter, and G. Wang,
J. Urol., 150, 1293–1297 (1993).
113. “Growth Inhibition of Hormone-Responsive and -Resistant Human Breast Cancer Cells in
Culture by N 1 ,N 12 -Bis(ethyl)spermine.” N. E. Davidson, A. R. Mank, L. J. Prestigiacomo,
R. J. Bergeron, and R. A. Casero, Jr., Cancer Res., 53, 2071–2075 (1993).
114. “A Comparative Study of the Iron-Clearing Properties of Desferrithiocin Analogs With
Desferrioxamine B in a Cebus Monkey Model.” R. J. Bergeron, R. R. Streiff, E. A. Creary,
R. D. Daniels, Jr., W. King, G. Luchetta, J. Wiegand, T. Moerker, and H. H. Peter, Blood,
81, 2166–2173 (1993).
115. “Antitumor Activity of N 1 ,N 11 -Bis(ethyl)norspermine Against Human Melanoma
Xenografts and Possible Biochemical Correlates of Drug Action.” C. W. Porter, R. J.
Bernacki, J. Miller, and R. J. Bergeron, Cancer Res., 53, 581–586 (1993).
116. “Investigations of the Mechanism by which Mammalian Cell Growth is Inhibited by N 1 ,N 12 -
Bis(ethyl)spermine.” L. Albanese, R. J. Bergeron, and A. E. Pegg, Biochem. J., 291, 131–
137 (1993).
117. “Toward Better Chelation Therapy: Current Concepts and Research Strategy.” H.-P.
Schnebli, I. Hassan, K. O. Hamilton, S. Lynch, Y. Jin, H. P. Nick, H. H. Peter, U. Junker
Walker, R. Ziel, S. C. Khanna, R. Dean, and R. J. Bergeron, The Development of Iron
Chelators for Clinical Use, CRC Press, Inc., Boca Raton, pp. 131–149 (1994).
118. “Synthesis and Biological Activity of Hydroxamate-Based Iron Chelators.” R. J.
Bergeron and J. S. McManis, The Development of Iron Chelators for Clinical Use, CRC
Press, Inc., Boca Raton, pp. 237–273 (1994).
119. “A Comparative Evaluation of Iron Chelators in a Primate Model.” H. H. Peter, R. J.
Bergeron, R. R. Streiff, and J. Wiegand, The Development of Iron Chelators for
Clinical Use, CRC Press, Inc., Boca Raton, pp. 373–394 (1994).
120. “A Comparison of the Iron-Clearing Properties of Parabactin and Desferrioxamine.”
R. J. Bergeron, R. R. Streiff, W. King, R. D. Daniels, Jr, and J. Wiegand, Blood, 82, 2552–
2557 (1993).
121. “Radiopotentiation of Human Brain Tumor Cells by the Spermine Analog N 1 ,N 14 -
Bis(ethyl)homospermine.” C.-Z. Chen, L. J. Hu, R. J. Bergeron, L. J. Marton, and D. F.
Deen, Int. J. Radiat. Oncol. Biol. Phys., 29, 1041–1047 (1994).
11

122. “Role of Ribonucleotide Reductase in Inhibition of Mammalian Cell Growth by Potent
Iron Chelators.” S. Nyholm, G. J. Mann, A. G. Johansson, R. J. Bergeron, A. Graslund, and
L. Thelander, J. Biol. Chem., 268, 26200–26205 (1993).
123. “Polyamine and Polyamine Analog Regulation of Spermidine/Spermine N 1
Acetyltransferase in MALME-3M Human Melanoma Cells.” M. Fogel-Petrovic, N. W.
Shappell, R. J. Bergeron, and C. W. Porter, J. Biol. Chem., 268, 19118–19125 (1993).
124. “Total Syntheses of (+)-Hypusine and Its (2S,9S)-Diastereomer.” R. J. Bergeron, M. X. B.
Xia, and O. Phanstiel, IV, J. Org. Chem., 58, 6804–6806 (1993).
125. “The Desferrithiocin Pharmacophore.” R. J. Bergeron, C. Z. Liu, J. S. McManis, M. X. B.
Xia, S. E. Algee, and J. Wiegand, J. Med. Chem., 37 (10), 1411–1417 (1994).
126. “A Versatile Synthesis of Desferrioxamine.” R.J. Bergeron, J. S. McManis, O. Phanstiel, IV,
and J. R. T. Vinson, J. Org. Chem., 60(1), 109–114 (1995).
127. “Antiproliferative Properties of Polyamine Analogues: A Structure-Activity Study.” R. J.
Bergeron, J. S. McManis, C. Z. Liu, Y. Feng, W. R. Weimar, G. R. Luchetta, Q. Wu, J.
Ortiz-Ocasio, J. R. T. Vinson, D. Kramer, and C. Porter, J. Med. Chem., 37(21), 3464–3476
(1994).
128. “Impact of Polyamine Analogues on the NMDA Receptor.” R. J. Bergeron, W. R.
Weimar, Q. Wu, J. K. Austin, Jr., and J. S. McManis, J. Med. Chem., 38, 425–428 (1995).
129. “An Investigation of Desferrithiocin Metabolism.” R. J. Bergeron, M. Wollenweber, and J.
Wiegand, J. Med. Chem., 37(18), 2889–2895 (1994).
130. “Macromolecular Self-Assembly of Diketopiperazine Tetrapeptides.” R. J. Bergeron, O.
Phanstiel, IV, G. W. Yao, S. Milstein, and W. R. Weimar, J. Am. Chem. Soc., 116(19),
8479–8484 (1994).
131. “Design and Testing of Novel Cytotoxic Polyamine Analogues.” H. S. Basu, L. J.
Marton, M. Pellarin, D. F. Deen, J. S. McManis, C. Z. Liu, R. J. Bergeron, and B. G.
Feuerstein, Cancer Res., 54, 6210–6214 (1994).
132. “Collateral Sensitivity of Human Melanoma Multidrug-resistant Variants to the
Polyamine Analogue, N 1 ,N 11 -Diethylnorspermine.” C. W. Porter, B. Ganis, Y. Rustum, C.
Wrzosek, D. L. Kramer, and R. J. Bergeron, Cancer Res., 54, 5917–5924 (1994).
133. “The Role of Charge in Polyamine Analogue Recognition.” R. J. Bergeron, J. S. McManis,
W. R. Weimar, K. Schreier, F. Gao, Q. Wu, J. Ortiz-Ocasio, G. R. Luchetta, C. Porter, and J.
R. T. Vinson, J. Med. Chem., 38, 2278–2285 (1995).
12

134. “An Investigation of the Impact of Molecular Geometry upon Microcapsule Self-
Assembly.” R. J. Bergeron, G. W. Yao, G. W. Erdos, S. Milstein, F. Gao, W. R. Weimar,
and O. Phanstiel, IV, J. Am. Chem. Soc., 117, 6658–6665 (1995).
135. “Metabolism and Pharmacokinetics of N 1 ,N 11 -Diethylnorspermine.” R. J. Bergeron, W. R.
Weimar, G. R. Luchetta, J. Wiegand, J. Perrin, K. Schreier, C. Porter, G. W. Yao, and H.
Dimova, Drug Met. Dispos., 23(10), 1117–1125 (1995).
136. “The Impact of Polyamine Analogues on the Blood Pressure of Normotensive and
Hypertensive Rats.” R. J. Bergeron, J. Wiegand, C. A. Sninsky, and M. J. Katovich,
Clin. Exper. Hypertension, 17(8), 1197–1217 (1995).
137. “Metabolism and Pharmacokinetics of N 1 ,N 14 -Diethylhomospermine.” R. J. Bergeron, W.
R. Weimar, G. R. Luchetta, C. A. Sninsky, R. R. Streiff, and J. Wiegand, Drug Met.
Dispos., 24(3), 334–343 (1996).
138. “Preclinical Antitumor Efficacy of the Polyamine Analogue N 1 ,N 11 -Diethylnorspermine
Administered by Multiple Injection or Continuous Infusion.” R. J. Bernacki, E. J.
Oberman, K. E. Seweryniak, A. Atwood, R. J. Bergeron, and C. W. Porter, Clin. Cancer
Res., 1, 847–857 (1995).
139. “Metabolically Programmed Polyamine Analogue Antidiarrheals.” R. J. Bergeron, G. W.
Yao, H. Yao, W. R. Weimar, C. A. Sninsky, B. Raisler, Y. Feng, Q. Wu, and F. Gao,
J. Med. Chem., 39(13), 2461–2471 (1996).
140. “Synthesis and Biological Evaluation of Naphthyldesferrithiocin Iron Chelators.” R. J.
Bergeron, J. Wiegand, M. Wollenweber, J. S. McManis, S. E. Algee, and K. Ratliff-
Thompson, J. Med. Chem., 39(8), 1575–1581 (1996).
141. “Polyamine Analogue Regulation of NMDA MK-801 Binding: A Structure–Activity
Study.” R. J. Bergeron, W. R. Weimar, Q. Wu, Y. Feng, and J. S. McManis, J. Med. Chem.,
39, 5257–5266 (1996).
142. “Total Synthesis of Rhizoferrin, An Iron Chelator.” R. J. Bergeron, M. G. Xin, R. E. Smith,
M. Wollenweber, J. S. McManis, C. Ludin, and K. A. Abboud, Tetrahedron, 53(2), 427–434
(1997).
143. “A Comparison of Structure–Activity Relationships between Spermidine and Spermine
Analogue Antineoplastics.” R. J. Bergeron, Y. Feng, W. R. Weimar, J. S. McManis, H.
Dimova, C. Porter, B. Raisler, and O. Phanstiel, J. Med. Chem., 40(10), 1475–1494 (1997).
144. “Development of a Hypusine Reagent for Peptide Synthesis.” R. J. Bergeron, C. Ludin,
R. Müller, R. E. Smith, and O. Phanstiel, IV, J. Org. Chem., 62(10), 3285–3290 (1997).
13

145. “Structural Basis for Differential Induction of Spermidine/Spermine N 1 -Acetyltransferase
Activity by Novel Spermine Analogs.” M. Fogel-Petrovic, D. L. Kramer, S. Vujcic, J.
Miller, J. S. McManis, R. J. Bergeron, and C. Porter, Mol. Pharmacol., 52, 69–74 (1997).
146. “Human Prostatic Carcinoma Cell Lines Display Altered Regulation of Polyamine
Transport in Response to Polyamine Analogs and Inhibitors.” Z. Mi, D. L. Kramer, J. T.
Miller, R. J. Bergeron, R. Bernacki, and C. W. Porter, The Prostate, 34, 51–60 (1998).
147. “The Origin of the Differences in (R)-and (S)-Desmethyldesferrithiocins: Iron-Clearing
Properties.” R. J. Bergeron, J. Wiegand, K. Ratliff-Thompson, and W. R. Weimar, Ann.
N. Y. Acad. Sci., 850, 202–216 (1998).
148. “The Influence of Molecular Conformation Upon the Self-Assembly of Cyclohexane
Diamide Diacids.” R. J. Bergeron, G. W. Yao, G. W. Erdos, S. Milstein, F. Gao, J. Rocca,
W. R. Weimar, H. L. Price, and O. Phanstiel, IV, Bioorg. Med. Chem., 5(11), 2049–2061
(1997).
149. “Effects of Novel Spermine Analogs on Cell Cycle Progression and Apoptosis in
MALME-3M Human Melanoma Cells.” D. L. Kramer, M. Fogel-Petrovic, P. Diegelman, J.
M. Cooley, J. S. McManis, R. J. Bergeron, and C. Porter, Cancer Res., 57, 5521–5527
(1997).
150. “Polyamine Analogue Antiarrhythmics.” R. J. Bergeron, J. Wiegand, W. R. Weimar, and P.
S. Snyder, Pharm. Res., 38(5), 367-380 (1998).
151. “HBED: A Potential Alternative to Deferoxamine for Iron-Chelating Therapy.” R. J.
Bergeron, J. Wiegand, and G. M. Brittenham, Blood, 91(4), 1446-1452 (1998).
152. “Lysosomal Sequestration of Polyamine Analogs in Chinese Hamster Ovary Cells Resistant
to the S-Adenosylmethionine Decarboxylase Inhibitor CGP-48664.” D. L. Kramer, J. D.
Black, H. Mett, R. J. Bergeron, and C. W. Porter, Cancer Res., 58, 3883–3890 (1998).
153. “Synthesis of Reagents for the Construction of Hypusine and Deoxyhypusine Peptides and
their Application as Peptidic Antigens.” R. J. Bergeron, W. R. Weimar, R. Müller, C. O.
Zimmerman, B. H. McCosar, H. Yao, and R. E. Smith, J. Med. Chem., 41(20), 3888-3900
(1998).
154. “Effect of Polyamine Analogues on Hypusine Content in JURKAT T-Cells.” R. J.
Bergeron, W. R. Weimar, R. Müller, C. O. Zimmerman, B. H. McCosar, H. Yao, and R.
E. Smith, J. Med. Chem., 41(20), 3901-3908 (1998).
155. “Desazadesmethyldesferrithiocin Analogues as Orally Effective Iron Chelators.” R. J.
Bergeron, J. Wiegand, W. R. Weimar, J. R. T. Vinson, J. Bussenius, G. W. Yao, and J.
S. McManis, J. Med. Chem., 42, 95–108 (1999).
14

156. “HBED: The Continuing Development of A Potential Alternative to Deferoxamine for
Iron-Chelating Therapy.” R. J. Bergeron, J. Wiegand, and G. M. Brittenham, Blood, 93(1),
370–375 (1999).
157. “Polyamine Analogue Induction of the p53-p21 WAF1CIP1 -Rb Pathway and G1 Arrest in
Human Melanoma Cells.” D. L. Kramer, S. Vujcic, P. Diegelman, J. Alderfer, J. T. Miller,
J. D. Black, R. J. Bergeron, and C. W. Porter, Cancer Res., 59, 1278–1286 (1999).
158. “Evaluation of the Desferrithiocin Pharmacophore as a Vector for Hydroxamates.” R. J.
Bergeron, J. S. McManis, J. Bussenius, G. M. Brittenham, and J. Wiegand, J. Med. Chem.,
42(15), 2881–2886 (1999).
159. “Effects of C-4 Stereochemistry and C-4' Hydroxylation on the Iron Clearing
Efficiency and Toxicity of Desferrithiocin Analogues.” R. J. Bergeron, J. Wiegand, J. S.
McManis, B. H. McCosar, W. R. Weimar, G. M. Brittenham, and R. E. Smith, J. Med.
Chem., 42, 2432–2440 (1999).
160. “A Search for Clinically Effective Iron Chelators.” R. J. Bergeron, J. S. McManis, J.
Wiegand, and W. R. Weimar, Iron Chelators: New Development Strategies, Saratoga
Publishing, Inc., Saratoga, pp. 253–292 (2000).
161. “(R)- and (S)-N-(Benzyloxycarbonyl)-3,4-epoxybutylamine. New 4-Amino-2-hydroxybutyl
Synthons for the Synthesis of Hypusine Reagents and (R)-6- and (S)-7-
Hydroxyspermidine.” R. J. Bergeron, J. Bussenius, R. Müller, B. H. McCosar, and J. S.
McManis, Tetrahedron: Asymmetry, 10(22), 4285–4294 (1999).
162. “Antimalarial Iron-Chelating Agents Based on Desferrithiocin.” G. M. Brittenham, R. J.
Bergeron, H. Fujioka, S. Looareesuwan, P. Wilairatana, P. Pootrakul, W.
Asawamahasakda, Y. Yuthavong, S. Meshnick, V. R. Gordeuk, and M. Aikawa, Measuring
the Impact of Tropical Diseases and Outcomes, U.S. Department of Health and Human
Services, National Institutes of Health, Bethesda, Maryland (1999).
163. “Pharmacokinetics of Orally Administered Desferrithiocin Analogs in Cebus apella
Primates.” R. J. Bergeron, W. R. Weimar, and J. Wiegand, Drug Metab. Dispos., 27(12),
1496–1498 (1999).
164. “Synthesis and Evaluation of Hydroxylated Polyamine Analogues as Antiproliferatives.” R.
J. Bergeron, R. Müller, J. Bussenius, J. S. McManis, R. L. Merriman, R. E. Smith, H.Yao,
and W. R. Weimar, J. Med. Chem., 43(2), 224–235 (2000).
165. “Metabolism and Pharmacokinetics of N 1 ,N 11 -Diethylnorspermine in a Cebus apella
Primate Model.” R. J. Bergeron, R. L. Merriman, S. G. Olson, J. Wiegand, J. Bender, R. R.
Streiff, and W. R. Weimar, Cancer Res., 60(16), 4433–4439 (2000).
166. “Complexation of Thorium(IV) with Desmethyldesferrithiocin.” L. Rao, G. R. Choppin,
and R. J. Bergeron, Radiochim. Acta, 88, 851–856 (2000).
15

167. “Polyamine Analogue Antidiarrheals: A Structure–Activity Study.” R. J. Bergeron, J.
Wiegand, J. S. McManis, W. R. Weimar, R. E. Smith, S. E. Algee, T. L. Fannin, M. A.
Slusher, and P. S. Snyder, J. Med. Chem., 44(2), 232–244 (2001).
168. “Synthesis and Evaluation of Hydroxylated Polyamine Analogues as Antiproliferatives.” R.
J. Bergeron, R. Müller, G. Huang, J. S. McManis, S. E. Algee, H. Yao, W. R. Weimar, and
J. Wiegand, J. Med. Chem., 44(15), 2451–2459 (2001).
169. “An Improved Synthesis of (3S,12S)-N 1 ,N 14 -Diethyl-3,12-dihydroxyhomospermine, a
Polyamine Analogue Therapeutic Agent.” R. J. Bergeron, R. Müller, J. S. McManis, G. W.
Yao, and G. Huang, Synthesis, 2001(7), 1043–1048 (2001).
170. “Significance of Asymmetric Sites in Choosing Siderophores as Deferration Agents.” R. J.
Bergeron, M. G. Xin, W. R. Weimar, R. E. Smith, and J. Wiegand, J. Med. Chem., 44(15),
2469-2478 (2001).
171. “HBED: Preclinical Studies of a Potential Alternative to Deferoxamine for Treatment of
Chronic Iron Overload and Acute Iron Poisoning.” R. J. Bergeron, J. Wiegand, and G. M.
Brittenham, Blood, 99(8), 3019-3026 (2002).
172. “Control of Irritable Bowel Syndrome with Polyamine Analogues: A Structure–Activity
Study.” R. J. Bergeron, J. Wiegand, and T. L. Fannin, Dig. Dis. Sci., 46(12), 2615–2623
(2001).
173. “Iron Chelators and Therapeutic Uses.” R. J. Bergeron, J. S. McManis, W. R. Weimar, J.
Wiegand, and E. Eiler-McManis, Burger’s Medicinal Chemistry, 6 th ed., Wiley, New York,
pp 479-561 (2003).
174. “Structure–Activity Relationships Among Desazadesferrithiocin Analogues.” R. J.
Bergeron, J. Wiegand, J. S. McManis, W. R. Weimar, and G. Huang, Iron Chelation
Therapy, Kluwer Academic/Plenum, New York, pp. 167–184 (2002).
175. “Measurement of Arsenic Bioavailability in Soil Using a Primate Model.” S. M. Roberts,
W. R. Weimar, J. R. T. Vinson, J. W. Munson, and R. J. Bergeron, Toxicol. Sci. 67, 303–
310 (2002).
176. “Hydroxylation of Desazadesferrithiocin Analogues: A Structure–Activity Study.” R. J.
Bergeron, Hematology 2001, American Society of Hematology, Washington, D. C.,
(Online at www.hematology.org, In Press 3/2002).
177. “Prevention of Acetic Acid-Induced Colitis by Desferrithiocin Analogs in a Rat Model.” R.
J. Bergeron, J. Wiegand, W. R. Weimar, J. N. Nguyen, and C. A. Sninsky, Dig. Dis. Sci.,
48(2), 399–407 (2003).
16

178. “Desferrithiocin Analogue-Based Hexacoordinate Iron(III) Chelators.” R. J. Bergeron, G.
Huang, W. R. Weimar, R. E. Smith, J. Wiegand, and J. S. McManis, J. Med. Chem., 46,
16–24 (2003).
179. “Methoxylation of Desazadesferrithiocin Analogues: Enhanced Iron Clearing Efficiency.”
R. J. Bergeron, J. Wiegand, J. S. McManis, J. Bussenius, R. E. Smith, and W. R. Weimar,
J. Med. Chem, 46, 1470–1477 (2003).
180. “Total Synthesis and Structure Revision of Petrobactin.” R. J. Bergeron, G. Huang, R. E.
Smith, N. Bharti, J. S. McManis, and A. Butler, Tetrahedron, 59(11), 2007–2014 (2003).
181. “Iron Chelation Promoted by Desazadesferrithiocin Analogs: An Enantioselective Barrier.”
R. J. Bergeron, J. Wiegand, W. R. Weimar, J. S. McManis, R. E. Smith, and K. A. Abboud,
Chirality, 15(7), 593–599 (2003).
182. “Polyamine–Iron Chelator Conjugate.” R. J. Bergeron, J. S. McManis, A. M. Franklin, H.
Yao, and W. R. Weimar, J. Med. Chem., 46(25), 5478–5483 (2003).
183. “Comparison of Iron Chelator Efficacy in Iron-Overloaded Beagle Dogs and
Monkeys.”(Cebus apella) R. J. Bergeron, J. Wiegand, W. R. Weimar, T. C. Lindstrom, T.
L. Fannin, and K. Ratliff-Thompson, Comparative Medicine, 54(6), 664–672 (2004).
184. “Impact of the Lipophilicity of Desferrithiocin Analogues on Iron Clearance.” R. J.
Bergeron, J. Wiegand, J. S. McManis, W. R. Weimar, J.H. Park, E. Eiler-McManis, J.
Bergeron, and G. M. Brittenham. ACS Symposium Series, Medicinal Inorganic Chemistry,
American Chemical Society, Washington, D.C., pp. 366–383, (2005).
185. “Partition-Variant Desferrithiocin Analogues: Organ Targeting and Increased Iron
Clearance.” R. J. Bergeron, J. Wiegand, J.S. McManis, W.R. Weimar, J.H. Park, E. Eiler-
McManis, J. Bergeron, and G. M. Brittenham, J. Med. Chem., 48(3), 821–831 (2005).
186. “Polyamine Vectored Iron Chelators: The Role of Charge.” R. J. Bergeron, N. Bharti, J.
Wiegand, J. S. McManis, H. Yao, and L. Prokai. J. Med. Chem., 48(12), 4120–4137
(2005).
187. “Synthesis and Biological Evaluation of Aminopolyamines.” R.J. Bergeron, G. Huang,
J. S. McManis, H. Yao, and J.N. Nguyen, J. Med.Chem., 48(9), 3099–3102 (2005).
188. “(S)-4,5-Dihydro-2-(2-hydroxy-4-hydroxyphenyl)-4-methyl-4-thiazolecarboxylic Acid
Polyethers: A Solution to Nephrotoxicity.” R. J. Bergeron, J. Wiegand, J.S. McManis,
J.R.T. Vinson, H. Yao, N. Bharti, and J. R. Rocca, J. Med.Chem., 49(9), 2772–2783
(2006) PubMed Central Manuscript #60988.
189. "The Design, Synthesis, and Evaluation of Organ-Specific Iron Chelators." R. J. Bergeron,
J. Wiegand, J. S. McManis, and N. Bharti, J. Med. Chem., 49(24), 7032–7043 (2006)
PubMed Central #61578.
17

190. "Total Synthesis of Vulnibactin: A Natural Product Chelator." R. J. Bergeron, N. Bharti,
and S. Singh, Synthesis, (7), 1033–1037 (2007).
191. "Impact of the 3,6,9-Trioxadecyloxy Group on Desazadesferrithiocin Analogue Iron
Clearance and Organ Distribution." R. J. Bergeron, J. Wiegand, N. Bharti, S. Singh, and J.
R. Rocca. J. Med. Chem., 50(14), 3302–3313 (2007) PubCentral Manuscript #62488.
192. "Design, Synthesis, and Testing of Non-Nephrotoxic Desazadesferrithiocin Polyether
Analogues." R. J. Bergeron, J. Wiegand, J. S. McManis, N. Bharti, and S. Singh. J. Med.
Chem., 51(13), 3913-23 (2008).
193. “Desferrithiocin Analogues and Nephrotoxicity.” R. J. Bergeron, J. Wiegand, J. S.
McManis, and N. Bharti, and S. Singh. J. Med. Chem., 51(19), 5993-6004 (2008).
194. “Desferrithiocin Analogue Uranium Decorporation Agents.” R. J. Bergeron, J. Wiegand, S.
Singh. Int. J. Radiat. Biol., 85 (4), 348-61 (2009).
195. “Vibriobactin Antibodies: A Vaccine Strategy.” R. J. Bergeron, N. Bharti, S. Singh, J. S.
McManis, J. Wiegand, L. G. Green. J. Med. Chem., 52 (12), 3801-13 (2009).
196. “The Impact of Polyether Chain Length on the Iron Clearing Efficiency and
Physiochemical Properties of Desferrithiocin Analogues.” R. J. Bergeron, N. Bharti, J.
Wiegand, J. S. McManis, S. Singh, K. A. Abboud. J. Med. Chem., 53 (7), 2843–2853
(2010).
197. “Design, Synthesis, and Testing of Polyamine Vectored Iron Chelators.” R. J. Bergeron, S.
Singh, N, Bharti, and Y. Jiang. Synthesis, 21, 3631-3636 (2010).
198. “Desferrithiocin analogue iron chelators: iron clearing efficiency, tissue distribution, and
renal toxicity” R. J. Bergeron, J. Wiegand, N. Bharti, J. S. McManis, and S. Singh.
Biometals, (24), 239–258 (2011).
199. “Synthesis of heterobactins A and B and Nocardia heterobactin.” R. J. Bergeron, S. Singh,
and N. Bharti. Tetrahedron, 67 (18), 3163-3169 (2011).
200. “Substituent Effects on Desferrithiocin and Desferrithiocin Analogue Iron-Clearing and
Toxicity Profiles.” R. J. Bergeron, J. Wiegand, N. Bharti, and J. S. McManis. J. Med.
Chem. (2012), 55(16), 7090-7103.
Books:
1. Iron Chelators: New Development Strategies. D. G. Badman, R. J. Bergeron, and G. M.
Brittenham, Eds. Saratoga Publishing, Inc., Saratoga, WY (2000).
18

2. The Development of Iron Chelators for Clinical Use. R. J. Bergeron and G. M. Brittenham,
Eds. CRC Press, Inc.: Boca Raton, FL (1994).
3. The Bioorganic Chemistry of Enzymatic Catalysis. M. L. Bender, R. J. Bergeron and M.
Komiyama. John Wiley and Sons: New York, NY (1984).
Patents:
1. “Methods and Intermediates for the Preparations of Spermidine, Homospermidine and
Norspermidine”
Patent No. 4,505,861 Issued 3/19/85
2. “Synthesis of Parabactin and Homologs Thereof”
Patent No. 4,565,874 Issued 1/21/86
3. “Methods for the Synthesis of Desferrioxamine B and Analogs Thereof”
Patent No. 4,987,253 Issued 1/22/91
4. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 5,091,576 Issued 2/25/92
5. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,128,353 Issued 7/09/92
6. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,173,505 Issued 12/22/92
7. “Improved Method of Synthesis of Desferrioxamine B, Analogs and Homologs Thereof”
Patent No. 5,254,724 Issued 10/19/93
8. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,292,775 Issued 3/8/94
9. “Analogs of Desferrioxamine B and Method for Synthesis Thereof”
Patent No. 5,322,961 Issued 6/21/94
10. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 5,342,945 Issued 8/30/94
11. “Analogues of Desferrioxamine B and Method for Synthesis Thereof”
Patent No. 5,364,965 Issued 11/15/94
12. “Method for Synthesis of Desferrioxamine B, Analogs and Homologs Thereof”
Patent No. 5,367,113 Issued 11/22/94
13. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,391,563 Issued 2/21/95
14. “Polyamine and Anti-Diarrheal and Gastrointestinal Anti-Spasmodic Pharmaceutical
Compositions and Methods of Treatment”
19

Patent No. 5,393,757 Issued 2/28/95
15. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 5,455,277 Issued 10/3/95
16. “Polyamines and Anti-Diarrheal and Gastrointestinal Anti-Spasmodic Pharmaceutical
Compositions and Methods of Treatment”
Patent No. 5,462,970 Issued 10/31/95
17. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,466,702 Issued 11/14/95
18. “Method for Preparing Desferrioxamine B and Homologs Thereof”
Patent No. 5,493,053 Issued 2/20/96
19. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,496,840 Issued 3/5/96
20. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,496,839 Issued 3/5/96
21. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,496,841 Issued 3/5/96
22. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,496,838 Issued 3/5/96
23. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,496,837 Issued 3/5/96
24. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,498,622 Issued 3/12/96
25. “Anti-Neoplastic Spermine Derivative”
European Patent No. 0 536 853 Issued 3/27/96 - U.S. Serial No. 06/936,835
26. “Anti-Hypertensive Composition and Methods of Treatment”
Patent No. 5,510,390 Issued 4/23/96
27. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,514,695 Issued 5/7/96
28. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,519,041 Issued 5/21/96
20

29. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,536,738 Issued 7/16/96
30. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,536,739 Issued 7/16/96
31. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,541,207 Issued 7/30/96
32. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,45,649 Issued 8/13/96
33. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,545,650 Issued 8/13/96
34. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,550,144 Issued 8/27/96
35. “Anti-Neoplastic, Anti-Viral and Ribonucleotide Reductase Activity Affecting
Pharmaceutical Compositions and Methods of Treatment”
Patent No. 5,569,666 Issued 10/29/96
36. “Sterically Hindered Tetraamines and Method for Their Production”
Patent No. 5,656,671 Issued 8/12/97
37. “Sterically Hindered Tetraamines and Method for Their Production”
Patent No. 5,677,351 Issued 10/14/97
38. “Polyamines and Anti-Diarrheal and Gastrointestinal Anti-Spasmodic Pharmaceutical
Compositions and Methods of Treatment”
Patent No. 5,677,352 Issued 10/14/97
39. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 5,679,682 Issued 10/21/97
40. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 5,681,837 Issued 10/28/97
41. “Method for Synthesis of Rhizoferrin”
Patent No. 5,739,395 Issued 4/14/98
42. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 5,827,894 Issued 10/27/98
43. “Thiazoline Acid Derivatives”
Patent No. 5,840,739 Issued 11/24/98
44. “Methods and Bicyclic Compositions for the Treatment of Inflammation”
Patent No. 5,843,959 Issued 12/1/98
21

45. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 5,866,613 Issued 2/2/99
46. “Sterically Hindered Tetraamines and Method for their Production”
Patent No. 5,886,050 Issued 3/23/99
47. “Methods and Compositions for the Treatment of Neurodegeneration”
Patent No. 5,886,051 Issued 3/23/99
48. “Hydroxy Polyamines”
Patent No. 5,962,533 Issued 10/5/99
49. “Hypusine Reagent for Peptide Synthesis”
Patent No. 5,973,113 Issued 10/26/99
50. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 6,034,139 Issued 3/7/00
51. “Thiazoline Acid Derivatives”
Patent No. 6,083,966 Issued 7/4/00
52. “Anti-Arrhythmic Compositions and Methods of Treatment”
Patent No. 6,083,991 Issued 7/4/00
53. “Anti-Neoplastic, Anti-Viral and Anti-Retroviral Spermine Derivatives”
Patent No. 6,147,262 Issued 11/14/00
54. “Method and Composition for Treatment of Inflammatory Bowel Disease”
Patent No. 6,159,983 Issued 12/12/00
55. “Chemical Resection of Pancreas”
Patent No. 6,160,022 Issued 12/12/00
56. “Analogs of Biologically Active, Naturally Occurring Polyamines, Pharmaceutical
Compositions and Methods of Treatment”
Patent No. 6,184,232 Issued 2/7/01
57. “Biologically Active Spermidine Analogues, Pharmaceutical Compositions and Methods
of Treatment”
Patent No. 6,235,794 Issued 5/22/01
58. “N,N'-Bis(2-hydroxybenzyl)ethylenediamine-N,N'-diacetic Acid in Iron Chelating
Therapy”
Patent No. 6,242,492 Issued 6/5/01
59. “Hypusine Reagent for Peptide Synthesis”
Patent No. 6,248,866 Issued 6/19/01
60. “Deoxyhypusine Reagent and Peptides”
Patent No. 6,258,931 Issued 7/10/01
61. “Sterically Hindered Tetraamines and Method for Their Production”
Patent No. 6,262,125 Issued 7/17/01
62. “Method of Inhibiting Biosynthesis of eIF-5A”
Patent No. 6,274,630 Issued 8/14/01
22

63. “Anti-Arrhythmic Compositions and Methods of Treatment”
Patent No. 6,297,287 Issued 10/2/01
64. “Analogs of Biologically Active, Naturally Occurring Polyamines, Pharmaceutical
Compositions and Methods of Treatment”
Patent No. 6,342,534 Issued 1/29/02
65. “Anti-Neoplastic, Anti-Viral or Anti-Retroviral Spermine Derivatives”
Patent No. 6,362,232 Issued 3/26/02
66. “Method and Composition for the Treatment of Diarrhea and Gastrointestinal Spasms”
Patent No. 6,399,662 Issued 6/4/02
67. “Polyamines and Anti-Diarrheal and Gastrointestinal Anti-Spasmodic Pharmaceutical
Compositions and Methods of Treatment”
Patent No. 6,455,591 Issued 9/24/02
68. “Method and Composition for Treatment of Irritable Bowel Disease”
Patent No. 6,458,795 Issued 10/1/02
69. “Sterically Hindered Tetraamines and Method for Their Production”
Patent No. 6,472,426 Issued 10/29/02
70. “Synthetic Hypusine Peptides”
Patent No. 6,492,489 Issued 12/10/02
71. “Method of Making Hypusine Peptides”
Patent No. 6,492,491 Issued 12/10/02
72. “Thiazoline Acid Derivatives”
Patent No. 6,521,652 Issued 2/18/03
73. “Thiazoline Acid Derivatives”
Patent No. 6,525,080 Issued 2/25/03
74. “N,N'-Bis(2-hydroxybenzyl)ethylenediamine-N,N'-diacetic Acid in Iron Chelating
Therapy”
Patent No. 6,531,510 Issued 3/11/03
75. “Thiazoline Acid Derivatives”
Patent No. 6,559,315 Issued 5/6/03
76. "Method and Composition for Treatment of Irritable Bowel Disease"
Patent No. 6,664,270 Issued 12/16/03
77. "Method and Composition for Treatment of Inflammatory Bowel Disease"
Patent No. 6,689,788 Issued 2/10/04
78. Method and Composition for Treatment of Irritable Bowel Disease”
Patent No. 6,818,656 Issued 11/16/04
79. Anti-Hypertensive Composition and Methods of Treatment”
Patent No. 6,841,576 Issued 1/11/05
80. “Iron Binding Agents”
Patent No. 6,864,270 Issued 3/08/05
23

81. "Analogs of Biologically Active, Naturally Occurring Polyamines, Pharmaceutical
Compositions and Methods of Treatment"
Patent No. 7,094,808 Issued 8/22/06
82. "Thiazoline Acid Derivatives"
Patent No. 7,126,004 Issued 10/24/06
83. “Iron Binding Agents”
Patent No. 7,144,904 Issued 12/05/06
84. “Aminopolyamine Sample Pharmacophores”
Patent No. 7,423,182 Issued 09/09/08
85. “Thiazoline Acid Derivatives”
Patent No. 7,531,563 Issued 05/12/09
86. “Anti-Hypertensive Composition and Method of Treatment”
Patent No. 7,691,684 Issued 04/06/10
87. “Iron Binding Agents”
Patent No. 7,879,886 Issued 2/01/2011
88. “Thiazoline Acid Derivatives”
Patent No. 8,008,502 Issued 8/30/2011
89. “Desferrithiocin Polyether Analogues”
Patent No. 8,278,458 Issued 10/02/2012
Revised 1/28/13
24